HG-10-102-01_product_DataBase

Bioactivity

HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research[1][2].

Target

IC50: 3.2 nM (LRRK2), 20.3 nM (wild-type LRRK2), 95.9 nM (LRRK2, 153.7 nM (LRRK2), 0.6 μM (MNK2), 2.1 μM (MLK1)

Invitro

HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant[1]. Western Blot Analysis[1] Cell Line:

In Vivo

HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice[1].HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure[1]. Animal Model:

Name

HG-10-102-01

CAS

1351758-81-0

Formula

C17H20ClN5O3

Molar Mass

377.83

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Choi HG, et al. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. [2]. Wang M, et al. Synthesis of [11C]HG-10-102-01 as a new potential PET agent for imaging of LRRK2 enzyme in Parkinson's disease. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1351-1355.

PeptideDB

HG-10-102-01

CAS: 1351758-81-0 F: C17H20ClN5O3 W: 377.83